Inhibitory Effects of Honokiol on the Voltage-Gated Potassium Channels in Freshly Isolated Mouse Dorsal Root Ganglion Neurons

被引:6
|
作者
Sheng, Anqi [1 ]
Zhang, Yan [1 ]
Li, Guang [2 ]
Zhang, Guangqin [1 ]
机构
[1] China Pharmaceut Univ, Dept Clin Pharm, Nanjing 210009, Jiangsu, Peoples R China
[2] Southwest Med Univ, Inst Cardiovasc Res, Key Lab Med Electrophysiol, Minist Educ, Luzhou 646000, Peoples R China
关键词
Honokiol; Dorsal root ganglion neurons; Patch clamp; Voltage-gated potassium channels; CHRONIC CONSTRICTION INJURY; KV1.4; ALPHA-SUBUNIT; MAGNOLIA-OFFICINALIS; AFFERENT NEURONS; SENSORY NEURONS; K+ CURRENTS; SPINAL-CORD; RAT; EXCITABILITY; MICE;
D O I
10.1007/s11064-017-2440-4
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Voltage-gated potassium (K-V) currents, subdivided into rapidly inactivating A-type currents (I-A) and slowly inactivating delayed rectifier currents (I-K), play a fundamental role in modulating pain by controlling neuronal excitability. The effects of Honokiol (Hon), a natural biphenolic compound derived from Magnolia officinalis, on K-V currents were investigated in freshly isolated mouse dorsal root ganglion neurons using the whole-cell patch clamp technique. Results showed that Hon inhibited I-A and I-K in concentration-dependent manner. The IC50 values for block of I-A and I-K were 30.5 and 25.7 mu M, respectively. Hon (30 mu M) shifted the steady-state activation curves of I-A and I-K to positive potentials by 17.6 and 16.7 mV, whereas inactivation and recovery from the inactivated state of I-A were unaffected. These results suggest that Hon preferentially interacts with the active states of the I-A and I-K channels, and has no effect on the resting state and inactivated state of the I-A channel. Blockade on K+ channels by Hon may contribute to its antinociceptive effect, especially anti-inflammatory pain.
引用
收藏
页码:450 / 457
页数:8
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